An inhibitor of JAK1 and TYK2
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PF-06700841 (tosylate)

Item No. 26125

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
[(1S)-2,2-difluorocyclopropyl][3-[2-[(1-methyl-1H-pyrazol-4-yl)amino]-4-pyrimidinyl]-3,8-diazabicyclo[3.2.1]oct-8-yl]-methanone, 4-methylbenzenesulfonate
CAS Number
2140301-96-6
Molecular Formula
C18H21F2N7O • C7H8O3S
Formula Weight
561.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlDMSO:PBS (pH 7.2) (1:20): 50µg/mlEthanol: slightly soluble
λmax
224 nm
SMILES
CN1N=CC(NC2=NC=CC(N3CC4CCC(N4C([C@H]5C(F)(F)C5)=O)C3)=N2)=C1.CC6=CC=C(S(O)(=O)=O)C=C6
InChi Code
InChI=1S/C18H21F2N7O.C7H8O3S/c1-25-8-11(7-22-25)23-17-21-5-4-15(24-17)26-9-12-2-3-13(10-26)27(12)16(28)14-6-18(14,19)20;1-6-2-4-7(5-3-6)11(8,9)10/h4-5,7-8,12-14H,2-3,6,9-10H2,1H3,(H,21,23,24);2-5H,1H3,(H,8,9,10)/t12?,13?,14-;/m0./s1
InChi Key
FAKGOYNHHHOTEN-WTMFEIAXSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $110

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    10 mg

    $186

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    25 mg

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    Product Description

    PF-06700841 is an inhibitor of JAK1 and tyrosine kinase 2 (TYK2; IC50s = 17 and 23 nM, respectively).1 It is selective for JAK1 and TYK2 over JAK2 and JAK3 (IC50s = 77 and 6,494 nM, respectively). PF-06700841 selectively inhibits IFN-α/STAT3 signaling over erythropoietin/STAT5 signaling in human whole blood (IC50s = 30 and 577 nM, respectively). It reduces increases in hind paw volume in a rat model of adjuvant-induced arthritis in a dose-dependent manner.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Fensome, A., Ambler, C.M., Arnold, E., et al. Dual inhibition of TYK2 and JAK1 for the treatment of autoimmune diseases: Discovery of ((S)-2,2-difluorocyclopropyl)((1R,5S)-3-(2-((1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841). J. Med. Chem. (2018).